Synthesis and comparative molecular field analysis (CoMFA) of antitumor 3-arylisoquinoline derivatives

Bioorg Med Chem. 1998 Dec;6(12):2449-58. doi: 10.1016/s0968-0896(98)80019-9.

Abstract

In this study a series of 3-arylisoquinoline derivatives were synthesized and cytotoxicity against human melanoma tumor cell evaluated, and a three dimensional quantitative structure-activity relationship was investigated using the comparative molecular field analysis (CoMFA). The results suggested that the electrostatic, steric and hydrophobic factors of 3-arylisoquinolines were strongly correlated with the antitumor activity. Considerable predictive ability (cross-validated r2 as high as 0.721) was obtained through CoMFA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Cell Survival / drug effects*
  • Computer Graphics
  • Humans
  • Indicators and Reagents
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / chemistry
  • Isoquinolines / toxicity
  • Melanoma
  • Models, Molecular
  • Molecular Structure
  • Regression Analysis
  • Reproducibility of Results
  • Static Electricity
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Indicators and Reagents
  • Isoquinolines